689251-97-6Relevant articles and documents
DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
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Paragraph 0710; 0713-0714, (2020/12/13)
The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.
Synthesis of 1-hetaryl-2,2-difluorocyclopropane-derived building blocks: The case of pyrazoles
Nosik, Pavel S.,Ryabukhin, Sergey V.,Pashko, Mykola O.,Grabchuk, Galyna P.,Grygorenko, Oleksandr O.,Volochnyuk, Dmitriy M.
, p. 80 - 89 (2018/12/04)
An approach to 1-hetaryl-2,2-difluorocyclopropane building blocks compatible with the current criteria of lead-oriented synthesis was developed and implemented for the case of 3-, 4- and 5-subsituted pyrazole derivatives. The method implied 6–9 synthetic steps, including difluorocyclopropanation with the TMSCF3–NaI system as the key transformation, and provided the title compounds on up to gram scale. The scope of the procedures towards substitution in the pyrazole ring and typical functional groups (i.e. COOH, NH2, CH2NH2, CH2OH) was established. The results obtained allowed formulation of preliminary guidelines for the synthetic feasibility of various functionalized 1-hetaryl-2,2-difluorocyclopropanes. 2018 Elsevier Ltd. All rights reserved.
AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
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Paragraph 0142, (2014/05/20)
The present invention relates to the filed of pharmarcutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) amd a preparation method thereof, a pharmarcutical composition with the compounds as active components, and a use of the azole compounds and the pharmarcutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as deinfed in the specifictaion.